ATE156482T1 - 1,4,5-TRIPHENYL-PYRAZOLE COMPOUNDS FOR TREATING INFLAMMATION AND INFLAMMATORY-RELATED DISORDERS - Google Patents

1,4,5-TRIPHENYL-PYRAZOLE COMPOUNDS FOR TREATING INFLAMMATION AND INFLAMMATORY-RELATED DISORDERS

Info

Publication number
ATE156482T1
ATE156482T1 AT95901779T AT95901779T ATE156482T1 AT E156482 T1 ATE156482 T1 AT E156482T1 AT 95901779 T AT95901779 T AT 95901779T AT 95901779 T AT95901779 T AT 95901779T AT E156482 T1 ATE156482 T1 AT E156482T1
Authority
AT
Austria
Prior art keywords
methyl
triphenyl
inflammatory
hydrido
trifluoromethyl
Prior art date
Application number
AT95901779T
Other languages
German (de)
Inventor
Len F Lee
Original Assignee
Searle & Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Searle & Co filed Critical Searle & Co
Application granted granted Critical
Publication of ATE156482T1 publication Critical patent/ATE156482T1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

A class of 1,4,5-triphenyl pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I <IMAGE> I wherein R1 is one or more groups independently selected from hydrido, methyl, ethyl, methoxy, ethoxy, methylthio, methylsulfinyl, methylsulfonyl, hydroxy, nitro, amino, N-methylamino, acetamido, trifluoromethyl, bromo, iodo, fluoro and chloro; wherein R2 is selected from hydrido, methyl, ethyl, cyano, trifluoromethyl, difluorochloromethyl, difluoromethyl, pentafluoroethyl and heptafluoropropyl; wherein R3 is one or more groups independently selected from hydrido, methyl, ethyl, methoxy, ethoxy, methylthio, methylsulfinyl, methylsulfonyl, hydroxy, nitro, amino, N-methylamino, acetamido, trifluoromethyl, bromo, iodo, fluoro and chloro; and wherein R4 is methyl; or a pharmaceutically-acceptable salt thereof.
AT95901779T 1993-11-30 1994-11-14 1,4,5-TRIPHENYL-PYRAZOLE COMPOUNDS FOR TREATING INFLAMMATION AND INFLAMMATORY-RELATED DISORDERS ATE156482T1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/161,004 US5401765A (en) 1993-11-30 1993-11-30 1,4,5-triphenyl pyrazolyl compounds for the treatment of inflammation and inflammation-related disorders

Publications (1)

Publication Number Publication Date
ATE156482T1 true ATE156482T1 (en) 1997-08-15

Family

ID=22579400

Family Applications (1)

Application Number Title Priority Date Filing Date
AT95901779T ATE156482T1 (en) 1993-11-30 1994-11-14 1,4,5-TRIPHENYL-PYRAZOLE COMPOUNDS FOR TREATING INFLAMMATION AND INFLAMMATORY-RELATED DISORDERS

Country Status (11)

Country Link
US (2) US5401765A (en)
EP (1) EP0731794B1 (en)
JP (1) JPH09505829A (en)
AT (1) ATE156482T1 (en)
AU (1) AU1088795A (en)
CA (1) CA2177573A1 (en)
DE (1) DE69404860T2 (en)
DK (1) DK0731794T3 (en)
ES (1) ES2105874T3 (en)
GR (1) GR3024939T3 (en)
WO (1) WO1995015317A1 (en)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5908852A (en) * 1994-11-14 1999-06-01 G. D. Searle & Co. 1,3,5 trisubstituted pyrazole compounds for treatment of inflammation
WO1996038418A1 (en) * 1995-06-02 1996-12-05 G.D. Searle & Co. Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US5643933A (en) * 1995-06-02 1997-07-01 G. D. Searle & Co. Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US5756529A (en) * 1995-09-29 1998-05-26 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies
CA2249009C (en) 1996-04-12 2003-09-16 G.D. Searle & Co. Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors
US6677364B2 (en) * 1998-04-20 2004-01-13 G.D. Searle & Co. Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US5677318A (en) * 1996-07-11 1997-10-14 Merck Frosst Canada, Inc. Diphenyl-1,2-3-thiadiazoles as anti-inflammatory agents
US6174330B1 (en) * 1997-08-01 2001-01-16 Schneider (Usa) Inc Bioabsorbable marker having radiopaque constituents
CA2327185A1 (en) * 1998-04-08 1999-10-14 Abbott Laboratories Pyrazole inhibitors of cytokine production
US6727238B2 (en) 1998-06-11 2004-04-27 Pfizer Inc. Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
US6294558B1 (en) 1999-05-31 2001-09-25 Pfizer Inc. Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
ES2222919T3 (en) * 1999-08-27 2005-02-16 Abbott Laboratories SULFONYL PHENYL PIRAZOLES USEFUL AS COX-2 INHIBITORS.
ATE252576T1 (en) 1999-12-03 2003-11-15 Pfizer Prod Inc HETEROARYLPHENYLPYRAZOLE COMPOUNDS FOR USE AS ANALGESIC/ANTI-INFLAMMATORY AGENT
PT1104760E (en) 1999-12-03 2003-06-30 Pfizer Prod Inc SULFAMOYL-HETEROARILPIRAZOLE COMPOUNDS AS ANALGESIC AND ANTI-INFLAMMATORY AGENTS
JP2003517475A (en) 1999-12-03 2003-05-27 ファイザー・プロダクツ・インク Heterocyclo-alkylsulfonylpyrazole derivatives as anti-inflammatory / analgesic agents
CA2326970C (en) 1999-12-03 2004-11-23 Pfizer Products Inc. Acetylene derivatives as anti-inflammatory/analgesic agents
AU784490B2 (en) * 1999-12-08 2006-04-13 Pharmacia Corporation Cyclooxygenase-2 inhibitor compositions having rapid onset of therapeutic effect
US20020183362A1 (en) * 2000-04-25 2002-12-05 Pharmacia Corporation 2-Fluorobenzenesulfonyl compounds for the treatment of inflammation
PE20020146A1 (en) * 2000-07-13 2002-03-31 Upjohn Co OPHTHALMIC FORMULATION INCLUDING A CYCLOOXYGENASE-2 (COX-2) INHIBITOR
AU5754701A (en) * 2000-07-13 2002-01-30 Pharmacia Corp Method of using cox-2 inhibitors in the treatment and prevention of ocular cox-2mediated disorders
US7115565B2 (en) * 2001-01-18 2006-10-03 Pharmacia & Upjohn Company Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability
MY137736A (en) 2001-04-03 2009-03-31 Pharmacia Corp Reconstitutable parenteral composition
US20030105144A1 (en) 2001-04-17 2003-06-05 Ping Gao Stabilized oral pharmaceutical composition
US6673818B2 (en) 2001-04-20 2004-01-06 Pharmacia Corporation Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation
DE60204823T2 (en) 2001-07-05 2005-12-29 Pfizer Products Inc., Groton Heterocyclo-alkylsulfonyl-pyrazoles as anti-inflammatory / analgesic agents
UA80682C2 (en) * 2001-08-06 2007-10-25 Pharmacia Corp Orally deliverable stabilized oral suspension formulation and process for the incresaing physical stability of thixotropic pharmaceutical composition
AR037090A1 (en) 2001-09-19 2004-10-20 Pharmacia Corp PIRAZOLILO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF INFLAMMATIONS
GT200200183A (en) 2001-09-28 2003-05-23 PROCEDURE TO PREPARE DERIVATIVES OF HETEROCICLOALQUILSULFONIL PIRAZOL
WO2003037336A1 (en) 2001-11-02 2003-05-08 Pfizer Products Inc. 1-(5-sulfonyl-pyridin-2-yl)-5-(methylidene-cycloalkylmethoxy)-1h-pyrazole-4-carbonitrile derivatives and other compounds as cyclooxygenase inhibitors for the treatment of arthritis, neurodegeneration and colon cancer
US7329401B2 (en) * 2002-04-15 2008-02-12 The Regents Of The University Of California Cyclooxygenase-2 selective agents useful as imaging probes and related methods
AU2003279622A1 (en) 2002-06-28 2004-01-19 Nitromed, Inc. Oxime and/or hydrazone containing nitrosated and/or nitrosylated cyclooxigenase-2 selective inhibitors, compositions and methods of use
PL1534305T3 (en) 2003-05-07 2007-03-30 Osteologix As Treating cartilage / bone conditions with water-soluble strontium salts
JP4745971B2 (en) * 2003-10-03 2011-08-10 ザ オハイオ ステート ユニバーシティー リサーチ ファウンデーション PDK-1 / Akt signaling inhibitor
US20060079566A1 (en) * 2003-10-03 2006-04-13 Ching-Shih Chen PDK-1/Akt signaling inhibitors
CN101626787A (en) * 2007-01-19 2010-01-13 马林克罗特公司 Diagnostic and therapeutic cyclooxygenase-2 binding ligands
US8039502B2 (en) 2007-07-24 2011-10-18 The Ohio State University Research Foundation Anti-infective agents against intracellular pathogens
US20120108823A1 (en) 2009-04-22 2012-05-03 The Ohio State University Research Foundation Anti-francisella agents
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1373212A (en) * 1970-12-07 1974-11-06 Wyeth John & Brother Ltd Pyrazole compounds
US3984431A (en) * 1972-03-15 1976-10-05 Claude Gueremy Derivatives of pyrazole-5-acetic acid
PH27357A (en) * 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
US5466823A (en) * 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides

Also Published As

Publication number Publication date
DE69404860T2 (en) 1998-01-02
US5401765A (en) 1995-03-28
CA2177573A1 (en) 1995-06-08
DE69404860D1 (en) 1997-09-11
EP0731794A1 (en) 1996-09-18
AU1088795A (en) 1995-06-19
GR3024939T3 (en) 1998-01-30
WO1995015317A1 (en) 1995-06-08
US5639777A (en) 1997-06-17
JPH09505829A (en) 1997-06-10
ES2105874T3 (en) 1997-10-16
EP0731794B1 (en) 1997-08-06
DK0731794T3 (en) 1998-03-09

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Legal Events

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REN Ceased due to non-payment of the annual fee